Patents Examined by Emily A Bernhardt
  • Patent number: 10370376
    Abstract: The present invention relates to an amorphous form of Idelalisib and its methods of preparation. Using a Cu-K? radiation, the X-ray powder diffraction (XRPD) pattern does not contain sharp diffraction peaks at a diffraction angle expressed in degrees 2?, and the X-ray powder diffraction pattern is shown in FIG. 1. The present invention also provides a preparation method for the amorphous form of Idelalisib. The amorphous form of Idelalisib of the present invention increases the solubility of Idelalisib and improves bioavailability of the drug product. As compared to the existing crystalline forms of Idelalisib, its solubility increases significantly, which improves body's absorption of the drug and makes it more efficacious in the clinical therapeutic treatment of diseases. Under the stress test conditions, the amorphous material can maintain good physical and chemical stabilities. The preparation method of amorphous Idelalisib according to the present invention is simple to operate and easy to implement.
    Type: Grant
    Filed: October 13, 2017
    Date of Patent: August 6, 2019
    Assignee: Alnova Pharmaceuticals, Ltd.
    Inventors: Xini Zhang, Zhigang Xiong, Tao Hu
  • Patent number: 10370340
    Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,
    Type: Grant
    Filed: April 26, 2018
    Date of Patent: August 6, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jérôme Emile Georges Guillemont, Patrice Palandjian, Marc René de Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen
  • Patent number: 10364218
    Abstract: A method of producing ?-caprolactam from 3-oxoadipic acid includes: step 1 of mixing at least one selected from the group consisting of 3-oxoadipic acid and salts thereof with a catalyst and a solvent in the presence of hydrogen to produce 3-hydroxyadipic acid; and step 2 of reacting the 3-hydroxyadipic acid which is a product of step 1, a salt or carboxylic acid derivative thereof, or a mixture of these with hydrogen and ammonia.
    Type: Grant
    Filed: September 8, 2016
    Date of Patent: July 30, 2019
    Assignee: Toray Industries, Inc.
    Inventors: Daijiro Tsukamoto, Masateru Ito, Katsushige Yamada, Kohei Yamashita, Masato Akahira, Koji Yamauchi
  • Patent number: 10364247
    Abstract: The invention provides novel compounds and methods of using such compounds to treat or prevent cancer.
    Type: Grant
    Filed: April 21, 2015
    Date of Patent: July 30, 2019
    Assignees: Ruijin Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Xiamen University, Brandeis University
    Inventors: Ruibao Ren, Xianming Deng, Ping Liu, Bo Jiao, Wei Huang
  • Patent number: 10357560
    Abstract: Disclosed is the use of fluorinated cyclic dinucleotides and pharmaceutically acceptable salts thereof as an adjuvant for the preparation of an oral vaccine. Further disclosed is the use of fluorinated cyclic dinucleotides and pharmaceutically acceptable salts thereof for enhancing the immune response to an orally administered vaccine.
    Type: Grant
    Filed: September 18, 2018
    Date of Patent: July 23, 2019
    Assignees: Brock University, National Research Council of Canada
    Inventors: Hongbin Yan, Wangxue Chen, Rhonda Kuo Lee
  • Patent number: 10358440
    Abstract: The present invention relates to Brexpiprazole having a purity of about 99.5% or more by area percentage of HPLC, having total impurities not more than 0.5% relative to brexpiprazole as measured by area percentage of HPLC, and having less than 0.1% 1-(benzo[b]thiophen-4-yl)piperazine or a salt thereof relative to brexpiprazole by area percentage of HPLC. The present invention also provides a composition comprising brexpiprazole having 1-(benzo[b]thiophen-4-yl)-piperazine or a salt thereof in an amount less than about 0.1% relative to brexpiprazole by area percentage of HPLC and process for the preparation of brexpiprazole.
    Type: Grant
    Filed: February 13, 2019
    Date of Patent: July 23, 2019
    Assignee: Cadila Healthcare Limited
    Inventors: Sanjay Jagdish Desai, Jayprakash Ajitsingh Parihar, Alpesh Pravinchandra Shah
  • Patent number: 10344029
    Abstract: The present disclosure provides compounds of structural Formula III: or a salt thereof, wherein Y is chosen from Further provided are pharmaceutical compositions comprising these compounds, and methods for treating cancer, such as pancreatic cancer or synovial sarcoma, using the compounds and compositions.
    Type: Grant
    Filed: August 24, 2018
    Date of Patent: July 9, 2019
    Assignee: Washington University
    Inventors: William Hawkins, Robert Mach, Dirk Spitzer, Suwanna Vangveravong, Brian Van Tine
  • Patent number: 10343998
    Abstract: The present invention relates to a new route of synthesis to obtain pharmaceutically acceptable Vismodegib. In addition, besides the synthesis also suitable pharmaceutical compositions and the use of the compound for the treatment of basal-cell carcinomas are disclosed.
    Type: Grant
    Filed: March 26, 2018
    Date of Patent: July 9, 2019
    Assignee: AZAD PHARMACEUTICAL INGREDIENTS AG
    Inventors: Christian Manfred Frech, Pasquale Gabriele Grieco, Christine Aebersold, Patrick Müller, Jan-Erik Ingenhoff, Miriam Oberholzer, Viktorya Rstakyan, Roman Gerber Aeschbacher
  • Patent number: 10344022
    Abstract: A compound of formula (II): or a compound of formula (IV): or a compound of formula (XX): is useful in the treatment of mycoses.
    Type: Grant
    Filed: September 24, 2018
    Date of Patent: July 9, 2019
    Assignee: PULMOCIDE LIMITED
    Inventors: Thomas Christopher Colley, Kazuhiro Ito, Garth Rapeport, Peter Strong, Peter John Murray, Stuart Thomas Onions, Mihiro Sunose
  • Patent number: 10336704
    Abstract: A method for preparing indenoisoquinoline derivatives represented by the following formula (I) is disclosed, which comprises the following steps: (A) providing a first reactant represented by the following formula (II) and a second reactant represented by the following formula (III): and (B) reacting the first reactant represented by the formula (II) and the second reactant represented by the formula (III) in a solvent and selectively adding R2NH2 therein, to obtain the indenoisoquinoline derivatives represented by the formula (I), wherein, R1, R2, R3, A, X, Y, Z, m and n are defined in the specification.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: July 2, 2019
    Assignee: NATIONAL TAIWAN NORMAL UNIVERSITY
    Inventor: Ching-Fa Yao
  • Patent number: 10336734
    Abstract: Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of ACK1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new ACK1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I are disclosed.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: July 2, 2019
    Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Nupam P. Mahajan, Kiran N. Mahajan, Nicholas J. Lawrence, Harshani R. Lawrence
  • Patent number: 10329266
    Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4 alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as oste
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: June 25, 2019
    Assignee: MEDIVIR AB
    Inventors: Lourdes Salvador Oden, Magnus Nilsson, Pia Kahnberg, Bertil Samuelsson, Urszula Grabowska
  • Patent number: 10329299
    Abstract: Provided herein are compounds of Formula (I?) or (A?), pharmaceutical compositions comprising the compounds, and methods of use thereof. The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including PI3 kinase activity.
    Type: Grant
    Filed: October 26, 2017
    Date of Patent: June 25, 2019
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Martin R. Tremblay
  • Patent number: 10323037
    Abstract: The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: June 18, 2019
    Assignee: JIANGSU HENGRUI MEDICINE CO., LTD.
    Inventors: Dong Liu, Minsheng Zhang, Qiyue Hu
  • Patent number: 10322108
    Abstract: Disclosed are a compound, a stereisomer and a tautomer thereof, a pharmaceutically acceptable salt thereof, and a solvate or a prodrug thereof, which can be used for preventing or treating a ROR? mediated disease. The compound has the structural formula (I).
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: June 18, 2019
    Assignee: Beijing Hanmi Pharmaceutical Co., Ltd.
    Inventors: Hai Xue, Tao Zhao, Mi Young Cha, Maengsup Kim
  • Patent number: 10323007
    Abstract: Described herein are quinazoline-based compounds and formulations thereof. In some embodiments, the compounds and/or formulations thereof can be effective to inhibit and/or kill A. baumannii. Also described herein are methods of treating a subject in need thereof by administering to the subject in need thereof a quinazoline-based compound and/or formulation thereof to the subject in need thereof.
    Type: Grant
    Filed: September 13, 2017
    Date of Patent: June 18, 2019
    Assignee: University of South Florida
    Inventors: Roman Manetsch, Kurt S. Van Horn, Whittney Burda, Lindsey N. Shaw, Renee Fleeman, Megan Barber, David Lawrence Flanigan
  • Patent number: 10322132
    Abstract: The present invention relates to the use of a compound of formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof, or a pharmaceutical composition containing the same in reducing uric acid level, preventing or reducing inflammations, and preventing or treating uratic or gouty diseases. In particular, the present invention relates to the use of a compound of formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof, or a pharmaceutical composition containing the same in the manufacture of a medicament for the treatment or prevention of hyperuricemia, gout, gouty inflammations, pain and uric acid nephropathy. R1 represents hydrogen, C1-4 alkyl or the like. R2 represents C1-10 alkyl or the like. R3 represents halogen or the like.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: June 18, 2019
    Assignee: SHANTON PHARMA CO., LTD
    Inventors: Qian Zhang, Zhenhua Huang, Jinrong Liu, Shuangshuang Chi
  • Patent number: 10308614
    Abstract: The present invention relates to compounds of formula (I): and salts thereof, wherein: R1-R4 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of BRG1, BRM and/or PB1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various BRG1-mediated disorders, BRM-mediated disorders and/or PB1-mediated disorders.
    Type: Grant
    Filed: August 24, 2017
    Date of Patent: June 4, 2019
    Assignees: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, Alexandre Cote, Terry Crawford, Martin Duplessis, Andrew Charles Good, Yves LeBlanc, Steven R. Magnuson, Christopher G. Nasveschuk, F. Anthony Romero, Yong Tang, Alexander M. Taylor
  • Patent number: 10308652
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: —(CR3R3)2-5-, —(CR3R3)x-Y—(CR3R3)y-, —Y—(CR3R3)2-3-Y—, —CR3R3-Y—(CR3R3)2-Y—, —Y—(CR3R3)2-Y—CR3R3-; and Y, R1, R2, R3, R5, R6, R8, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: June 4, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Gregory D. Brown, Shuqun Lin, Jingwu Duan, Zhonghui Lu, Murali T. G. Dhar, Hai-Yun Xiao, Andrew J. Tebben
  • Patent number: 10301271
    Abstract: The disclosure relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzoate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: May 28, 2019
    Assignee: Purdue Pharma L.P.
    Inventors: Jay Jie-Qiang Wu, Ling Wang